JP2014521735A5 - - Google Patents
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- Publication number
- JP2014521735A5 JP2014521735A5 JP2014525437A JP2014525437A JP2014521735A5 JP 2014521735 A5 JP2014521735 A5 JP 2014521735A5 JP 2014525437 A JP2014525437 A JP 2014525437A JP 2014525437 A JP2014525437 A JP 2014525437A JP 2014521735 A5 JP2014521735 A5 JP 2014521735A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- condition
- disease
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 9
- 239000011780 sodium chloride Substances 0.000 claims 9
- 201000010099 disease Diseases 0.000 claims 4
- 102000001805 Bromodomains Human genes 0.000 claims 2
- 108050009021 Bromodomains Proteins 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- FICAQKBMCKEFDI-UHFFFAOYSA-N 3,5-dimethyl-1,2-oxazole Chemical compound CC=1C=C(C)ON=1 FICAQKBMCKEFDI-UHFFFAOYSA-N 0.000 claims 1
- HYPXHDJBILNWLI-CQSZACIVSA-N 4-[8-methoxy-1-[(2R)-1-methoxypropan-2-yl]-2-(oxan-4-yl)imidazo[4,5-c]quinolin-7-yl]-3,5-dimethyl-1,2-oxazole Chemical compound COC1=CC2=C3N([C@H](C)COC)C(C4CCOCC4)=NC3=CN=C2C=C1C=1C(C)=NOC=1C HYPXHDJBILNWLI-CQSZACIVSA-N 0.000 claims 1
- HYPXHDJBILNWLI-AWEZNQCLSA-N 4-[8-methoxy-1-[(2S)-1-methoxypropan-2-yl]-2-(oxan-4-yl)imidazo[4,5-c]quinolin-7-yl]-3,5-dimethyl-1,2-oxazole Chemical compound COC1=CC2=C3N([C@@H](C)COC)C(C4CCOCC4)=NC3=CN=C2C=C1C=1C(C)=NOC=1C HYPXHDJBILNWLI-AWEZNQCLSA-N 0.000 claims 1
- -1 8-methoxy-1- (1-methoxypropan-2-yl) -2- (tetrahydro-2H-pyran-4-yl) -1H-imidazo [4,5-c] quinolin-7-yl Chemical group 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000001684 chronic Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1114103.3 | 2011-08-17 | ||
| GBGB1114103.3A GB201114103D0 (en) | 2011-08-17 | 2011-08-17 | Novel compounds |
| PCT/EP2012/065918 WO2013024104A1 (en) | 2011-08-17 | 2012-08-15 | 4-(8-methoxy-1-((1-methoxypropan-2-yl)-2-(tetrahydro-2h-pyran-4-yl)-1 h-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazole and its use as bromodomain inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014521735A JP2014521735A (ja) | 2014-08-28 |
| JP2014521735A5 true JP2014521735A5 (de) | 2015-09-10 |
| JP6059723B2 JP6059723B2 (ja) | 2017-01-11 |
Family
ID=44764570
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014525437A Expired - Fee Related JP6059723B2 (ja) | 2011-08-17 | 2012-08-15 | ４−（８−メトキシ−１−（（１−メトキシプロパン−２−イル）−２−（テトラヒドロ−２Ｈ−ピラン−４−イル）−１Ｈ−イミダゾ［４，５−ｃ］キノリン−７−イル）−３，５−ジメチルイソオキサゾールおよびブロモドメイン阻害剤としてのその使用 |
Country Status (37)
| Country | Link |
|---|---|
| US (4) | US9067936B2 (de) |
| EP (2) | EP2744809B1 (de) |
| JP (1) | JP6059723B2 (de) |
| KR (1) | KR20140064878A (de) |
| CN (1) | CN103889984B (de) |
| AR (1) | AR087545A1 (de) |
| AU (1) | AU2012296914B2 (de) |
| BR (1) | BR112014003681A8 (de) |
| CA (1) | CA2843537A1 (de) |
| CL (1) | CL2014000365A1 (de) |
| CO (1) | CO6862151A2 (de) |
| CR (1) | CR20140076A (de) |
| CY (1) | CY1118370T1 (de) |
| DK (1) | DK2744809T3 (de) |
| DO (1) | DOP2014000031A (de) |
| EA (1) | EA023374B1 (de) |
| ES (1) | ES2609857T3 (de) |
| GB (1) | GB201114103D0 (de) |
| HR (1) | HRP20161674T1 (de) |
| HU (1) | HUE030106T2 (de) |
| IL (1) | IL230489A (de) |
| IN (1) | IN2014CN00568A (de) |
| JO (1) | JO3187B1 (de) |
| LT (1) | LT2744809T (de) |
| ME (1) | ME02589B (de) |
| MX (1) | MX350597B (de) |
| MY (1) | MY170729A (de) |
| PE (1) | PE20141406A1 (de) |
| PL (1) | PL2744809T3 (de) |
| PT (1) | PT2744809T (de) |
| RS (1) | RS55560B1 (de) |
| SI (1) | SI2744809T1 (de) |
| SM (1) | SMT201700005B (de) |
| TW (1) | TWI558704B (de) |
| UA (1) | UA110838C2 (de) |
| UY (1) | UY34264A (de) |
| WO (1) | WO2013024104A1 (de) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| US9249161B2 (en) | 2010-12-02 | 2016-02-02 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| US9422292B2 (en) | 2011-05-04 | 2016-08-23 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| WO2012174487A2 (en) | 2011-06-17 | 2012-12-20 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| GB201114103D0 (en) * | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
| TWI602820B (zh) | 2012-06-06 | 2017-10-21 | 星宿藥物公司 | 溴域抑制劑及其用途 |
| EP2864336B1 (de) | 2012-06-06 | 2016-11-23 | Constellation Pharmaceuticals, Inc. | Benzo[b]isoxazolazepinbromdomänenhemmer und verwendungen davon |
| WO2014080291A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Biaryl derivatives as bromodomain inhibitors |
| WO2014080290A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Cyclic amines as bromodomain inhibitors |
| CA2895905A1 (en) | 2012-12-21 | 2014-06-26 | Zenith Epigenetics Corp. | Novel heterocyclic compounds as bromodomain inhibitors |
| AU2014249192B2 (en) | 2013-03-11 | 2017-12-21 | The Regents Of The University Of Michigan | BET bromodomain inhibitors and therapeutic methods using the same |
| EP2970285B1 (de) | 2013-03-11 | 2019-04-17 | AbbVie Inc. | Tetracyclische kondensierte bromodomänenhemmer |
| WO2014164771A1 (en) * | 2013-03-11 | 2014-10-09 | Abbvie Inc. | Bromodomain inhibitors |
| SG10201707487VA (en) | 2013-03-15 | 2017-10-30 | Incyte Corp | Tricyclic heterocycles as bet protein inhibitors |
| TWI530499B (zh) * | 2013-03-28 | 2016-04-21 | 吉李德科學股份有限公司 | 作為溴結構域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑之苯並咪唑酮衍生物類 |
| NZ714669A (en) | 2013-06-21 | 2021-07-30 | Zenith Epigenetics Ltd | Novel bicyclic bromodomain inhibitors |
| JP6461118B2 (ja) | 2013-06-21 | 2019-01-30 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメイン阻害剤としての新規の置換された二環式化合物 |
| WO2015006193A1 (en) | 2013-07-08 | 2015-01-15 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| EA201690087A1 (ru) | 2013-07-31 | 2016-08-31 | Зенит Эпидженетикс Корп. | Новые квиназолиноны как ингибиторы бромодомена |
| WO2015049629A1 (en) * | 2013-10-01 | 2015-04-09 | Piramal Enterprises Limited | Imidazoquinoline compounds as bromodomain inhibitors |
| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| CN107074861A (zh) | 2014-02-28 | 2017-08-18 | 密执安大学评议会 | 作为bet溴结构域抑制剂的9h嘧啶并[4，5‑b]吲哚和相关类似物 |
| SG11201608843TA (en) | 2014-04-23 | 2016-11-29 | Incyte Corp | 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS |
| EP3157928B1 (de) | 2014-06-20 | 2019-02-13 | Constellation Pharmaceuticals, Inc. | Kristalline formen von 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamid |
| WO2016044130A1 (en) | 2014-09-15 | 2016-03-24 | Incyte Corporation | Tricyclic heterocycles for use as bet protein inhibitors |
| CA2966303A1 (en) | 2014-12-01 | 2016-06-09 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| WO2016087936A1 (en) | 2014-12-01 | 2016-06-09 | Zenith Epigenetics Corp. | Substituted pyridinones as bromodomain inhibitors |
| CA2966449A1 (en) | 2014-12-11 | 2016-06-16 | Zenith Epigenetics Ltd. | Substituted heterocycles as bromodomain inhibitors |
| CN107406438B (zh) | 2014-12-17 | 2021-05-14 | 恒翼生物医药科技(上海)有限公司 | 溴结构域的抑制剂 |
| WO2016123709A1 (en) * | 2015-02-03 | 2016-08-11 | Trillium Therapeutics Inc. | Fluorinated imidazo[4,5-c]quinoline derivatives as inhibitors of bromodomain containing proteins |
| EP3262045A1 (de) | 2015-02-27 | 2018-01-03 | The Regents of The University of Michigan | 9h-pyrimido[4,5-b]indole als bet-bromdomänen-hemmer |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| GB201504689D0 (en) * | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| WO2016186453A1 (en) * | 2015-05-20 | 2016-11-24 | Kainos Medicine, Inc. | Quinoline derivatives as bromodomain inhibitors |
| WO2016196065A1 (en) | 2015-05-29 | 2016-12-08 | Genentech, Inc. | Methods and compositions for assessing responsiveness of cancers to bet inhibitors |
| WO2016199943A1 (en) * | 2015-06-11 | 2016-12-15 | Takeda Pharmaceutical Company Limited | Heterocyclic compounds |
| US10836742B2 (en) | 2015-08-11 | 2020-11-17 | Neomed Institute | N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals |
| KR20180039117A (ko) | 2015-08-11 | 2018-04-17 | 네오메드 인스티튜트 | 아릴-치환된 디히드로퀴놀리논, 그의 제조법 및 제약으로서의 그의 용도 |
| EP3334719B1 (de) | 2015-08-12 | 2021-09-15 | Neomed Institute | Substituierte benzimidazole, deren herstellung und deren verwendung als pharmazeutika |
| WO2017066876A1 (en) | 2015-10-21 | 2017-04-27 | Neomed Institute | Substituted imidazopyridines, their preparation and their use as pharmaceuticals |
| US20170121347A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| WO2017127930A1 (en) | 2016-01-28 | 2017-08-03 | Neomed Institute | Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals |
| WO2017142881A1 (en) | 2016-02-15 | 2017-08-24 | The Regents Of The University Of Michigan | Fused 1,4-oxazepines and related analogs as bet bromodomain inhibitors |
| US11192898B2 (en) | 2016-04-06 | 2021-12-07 | The Regents Of The University Of Michigan | MDM2 protein degraders |
| CA3020281A1 (en) | 2016-04-06 | 2017-10-12 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| RU2752677C2 (ru) | 2016-04-12 | 2021-07-29 | Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган | Деструкторы белка вет |
| IL263824B2 (en) | 2016-06-20 | 2023-10-01 | Incyte Corp | Crystals in solid form in the presence of an inhibitor |
| EP3858837A1 (de) | 2016-09-13 | 2021-08-04 | The Regents of The University of Michigan | Kondensierte 1,4-diazepine als bet-protein-abbauer |
| WO2018052945A1 (en) | 2016-09-13 | 2018-03-22 | The Regents Of The University Of Michigan | Fused 1,4-oxazepines as bet protein degraders |
| US11046709B2 (en) | 2017-02-03 | 2021-06-29 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as BET bromodomain inhibitors |
| WO2019055444A1 (en) | 2017-09-13 | 2019-03-21 | The Regents Of The University Of Michigan | DEGRADATION AGENTS OF BROMODOMAIN BET PROTEIN WITH CLEAR BINDERS |
| CN108033957A (zh) * | 2018-01-09 | 2018-05-15 | 中国药科大学 | 一种喹啉类BET bromodomain抑制剂及其制备方法和用途 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| WO2022132049A1 (en) * | 2020-12-17 | 2022-06-23 | National University Of Singapore | Treating cancers using bet inhibitors |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9004781D0 (en) | 1990-03-02 | 1990-04-25 | Glaxo Group Ltd | Device |
| GB0211649D0 (en) | 2002-05-21 | 2002-07-03 | Novartis Ag | Organic compounds |
| EP1590348A1 (de) | 2002-12-20 | 2005-11-02 | 3M Innovative Properties Company | Aryl / hetaryl-substituierte imidazochinoline |
| BRPI0416128B8 (pt) | 2003-11-03 | 2021-06-22 | Glaxo Group Ltd | dispositivo de dispensação de fluido |
| KR20060117329A (ko) | 2003-11-21 | 2006-11-16 | 노파르티스 아게 | 단백질 키나제 저해제로서의 1ｈ-이미다조퀴놀린 유도체 |
| US8658666B2 (en) | 2005-02-11 | 2014-02-25 | 3M Innovative Properties Company | Substituted imidazoquinolines and imidazonaphthyridines |
| KR20080048551A (ko) | 2005-09-23 | 2008-06-02 | 콜레이 파마시티컬 그룹, 인코포레이티드 | 1Ｈ-이미다조[4,5-ｃ]피리딘 및 그의 유사체의 제조법 |
| CN101330916A (zh) | 2005-12-16 | 2008-12-24 | 科勒制药集团公司 | 经取代的咪唑并喹啉、咪唑并萘啶和咪唑并吡啶、其组合物及其方法 |
| JP2008156311A (ja) | 2006-12-26 | 2008-07-10 | Institute Of Physical & Chemical Research | Ｂｒｄ２ブロモドメイン結合剤 |
| WO2009084693A1 (ja) | 2007-12-28 | 2009-07-09 | Mitsubishi Tanabe Pharma Corporation | 抗癌剤 |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| WO2011054845A1 (en) * | 2009-11-05 | 2011-05-12 | Glaxosmithkline Llc | Benzodiazepine bromodomain inhibitor |
| GB0919432D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| GB0919434D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB201106799D0 (en) * | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201114103D0 (en) | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
-
2011
- 2011-08-17 GB GBGB1114103.3A patent/GB201114103D0/en not_active Ceased
-
2012
- 2012-08-15 DK DK12748028.3T patent/DK2744809T3/en active
- 2012-08-15 PE PE2014000167A patent/PE20141406A1/es not_active Application Discontinuation
- 2012-08-15 WO PCT/EP2012/065918 patent/WO2013024104A1/en active Application Filing
- 2012-08-15 CN CN201280040092.5A patent/CN103889984B/zh not_active Expired - Fee Related
- 2012-08-15 EA EA201490200A patent/EA023374B1/ru not_active IP Right Cessation
- 2012-08-15 HU HUE12748028A patent/HUE030106T2/en unknown
- 2012-08-15 LT LTEP12748028.3T patent/LT2744809T/lt unknown
- 2012-08-15 MX MX2014001834A patent/MX350597B/es active IP Right Grant
- 2012-08-15 EP EP12748028.3A patent/EP2744809B1/de active Active
- 2012-08-15 BR BR112014003681A patent/BR112014003681A8/pt not_active Application Discontinuation
- 2012-08-15 KR KR1020147007082A patent/KR20140064878A/ko not_active Application Discontinuation
- 2012-08-15 UY UY0001034264A patent/UY34264A/es not_active Application Discontinuation
- 2012-08-15 MY MYPI2014700328A patent/MY170729A/en unknown
- 2012-08-15 UA UAA201400590A patent/UA110838C2/uk unknown
- 2012-08-15 PL PL12748028T patent/PL2744809T3/pl unknown
- 2012-08-15 ME MEP-2016-288A patent/ME02589B/de unknown
- 2012-08-15 CA CA2843537A patent/CA2843537A1/en not_active Abandoned
- 2012-08-15 SI SI201230818A patent/SI2744809T1/sl unknown
- 2012-08-15 ES ES12748028.3T patent/ES2609857T3/es active Active
- 2012-08-15 EP EP16192662.1A patent/EP3150601A1/de not_active Withdrawn
- 2012-08-15 TW TW101129613A patent/TWI558704B/zh not_active IP Right Cessation
- 2012-08-15 IN IN568CHN2014 patent/IN2014CN00568A/en unknown
- 2012-08-15 AR ARP120102987A patent/AR087545A1/es unknown
- 2012-08-15 RS RS20170014A patent/RS55560B1/sr unknown
- 2012-08-15 AU AU2012296914A patent/AU2012296914B2/en not_active Ceased
- 2012-08-15 JP JP2014525437A patent/JP6059723B2/ja not_active Expired - Fee Related
- 2012-08-15 PT PT127480283T patent/PT2744809T/pt unknown
- 2012-08-15 US US14/237,905 patent/US9067936B2/en not_active Expired - Fee Related
- 2012-08-15 JO JOP/2012/0229A patent/JO3187B1/ar active
-
2014
- 2014-01-16 IL IL230489A patent/IL230489A/en active IP Right Grant
- 2014-01-21 CO CO14011125A patent/CO6862151A2/es not_active Application Discontinuation
- 2014-02-13 CL CL2014000365A patent/CL2014000365A1/es unknown
- 2014-02-17 DO DO2014000031A patent/DOP2014000031A/es unknown
- 2014-02-17 CR CR20140076A patent/CR20140076A/es unknown
-
2015
- 2015-05-28 US US14/723,556 patent/US9416130B2/en not_active Expired - Fee Related
-
2016
- 2016-07-08 US US15/205,372 patent/US9610284B2/en not_active Expired - Fee Related
- 2016-12-08 HR HRP20161674TT patent/HRP20161674T1/hr unknown
- 2016-12-16 CY CY20161101310T patent/CY1118370T1/el unknown
-
2017
- 2017-01-04 SM SM201700005T patent/SMT201700005B/it unknown
- 2017-02-17 US US15/435,697 patent/US9861627B2/en not_active Expired - Fee Related
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